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Diaziquone

Diaziquone

产品编号 T61383   CAS 57998-68-2
别名: NSC 182986

Diaziquone (NSC-182986)是一种水溶性的合成的氮杂环苯醌,可增强对血脑屏障的渗透,具有抗肿瘤活性,可用于治疗极性肾功能衰竭。

TargetMol的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
Diaziquone Chemical Structure
Diaziquone, CAS 57998-68-2
规格 价格/CNY 货期 数量
1 mg ¥ 1,320 现货
5 mg ¥ 3,300 现货
10 mg ¥ 4,790 现货
25 mg ¥ 7,580 现货
50 mg ¥ 9,870 现货
100 mg ¥ 13,700 现货
500 mg ¥ 27,600 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Diaziquone (T61383)
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纯度: 98.37%
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生物活性
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存储 & 溶解度
参考文献
产品描述 Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure.
体外活性 Diaziquone (5000 ng/mL) is associated with prolonged aplasia and rare instances of bone marrow necrosis, but only mild extramedullary toxicity. One- and three-hour treatments produced little cytotoxicity for hematopoietic versus marrow stromal cells. After six-hour treatments with this dose, marrow was depleted of CFU-Mix, BFU-E, and CFU-GM, but produced CFU-GM in LTMCs, indicating an ongoing input of CFU-GM from a surviving pre-CFU-Mix population. Diaziquone (150 ng/mL; 3 to 7 days) elimination of the latter may be inferred from the absence of CFU-GM in the LTMCs exposed.[4]
体内活性 Diaziquone (0.1 mg/day; injection; 4 days) applied topically in Vanicream, Plastibase, or DMSO inhibited tumor growth at day 20 by 66, 86, and 43%, respectively, and cured animals of the skin tumor at a dose of 0.5 mg/day. Diaziquone administered i.p. at 0.5 mg/day for 4 days was lethal to rats, and at 0.1 mg/day it produced 93% inhibition of tumor growth at day 20. Diaziquone was applied topically at 0.1 mg/day for 4 days in Plastibase-cured rats of advanced tumors when treatment was begun 12 days after injection of tumor cells. The area under the plasma radioactivity time curve over 5 h for a single 0.64-mg dose of topically applied [ring-14C]diaziquone in DMSO was 0.01% that of the same dose of [ring-14C]diaziquone administered i.p. in non-tumored rats. The decrease in WBC count following topical application of diaziquone at a dose of 0.1 mg/day for 4 days, compared to the same dose of diaziquone administered i.p., was 62% in Vanicream, 81% in Plastibase and 33% in DMSO. Topical diaziquone was non-toxic to normal skin in the rat and in the domestic pig. It is concluded that topical application of diaziquone offers a therapeutic advantage over systemic treatment for metastatic cancer of the skin.[2]
别名 NSC 182986
分子量 364.35
分子式 C16H20N4O6
CAS No. 57998-68-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 45 mg/mL (123.51 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7446 mL 13.7231 mL 27.4461 mL 68.6153 mL
5 mM 0.5489 mL 2.7446 mL 5.4892 mL 13.7231 mL
10 mM 0.2745 mL 1.3723 mL 2.7446 mL 6.8615 mL
20 mM 0.1372 mL 0.6862 mL 1.3723 mL 3.4308 mL
50 mM 0.0549 mL 0.2745 mL 0.5489 mL 1.3723 mL
100 mM 0.0274 mL 0.1372 mL 0.2745 mL 0.6862 mL

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TargetMol Library Books参考文献

1. Schold SC Jr, et al. Treatment of human glioma and medulloblastoma tumor lines in athymic mice with diaziquone and diaziquone-based drug combinations. Cancer Res. 1984;44(6):2352-2357. 2. Moore DJ, et al. Topical chemotherapy of intradermal Walker 256 carcinosarcoma with diaziquone and doxorubicin in the rat. Cancer Res. 1985;45(11 Pt 1):5466-5472. 3. Lee EJ, et al. Diaziquone given as a continuous infusion is an active agent for relapsed adult acute nonlymphocytic leukemia. Blood. 1986;67(1):182-187. 4. Kushner BH, et al. Myeloablation with diaziquone: in vitro assessment. Blood. 1987;69(6):1747-1752. 5. Gutierrez PL, et al. Free radicals in quinone containing antitumor agents. The nature of the diaziquone (3,6,-diaziridinyl-2,5-bis(carboethoxyamino)-1,4-benzoquinone) free radical. Biochim Biophys Acta. 1983;758(1):37-41. 6. White L. Responsiveness of retinoblastoma to local diaziquone. Studies in a xenograft model. Invest Ophthalmol Vis Sci. 1990;31(5):787-791.

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌化合物库 经典已知活性库 已知活性化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Diaziquone 57998-68-2 NSC 182986 NSC-182986 NSC182986 Inhibitor inhibitor inhibit

 

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